Xiao-shu He

The role of novel ligands in the biological characterization of sigma receptors

Publisher Summary This chapter discusses the role of novel ligands in the biological characterization of sigma receptors. Investigation of the physiological and pharmacological role of sigma receptors is a relatively new area that has been facilitated by the development of high affinity and selective sigma receptor ligands including putative agonists and antagonists. Many different classes of drugs, ranging from steroids such as progesterone to neuroleptics such as haloperidol, exhibit high affinity for sigma receptors. This binding activity of the neuroleptic drugs suggested that sigma receptors may be responsible, at least in part, for the motor side-effects of these drugs. Sigma receptor research has been greatly facilitated by the development of chemical tools ranging from antagonists that allow the probing of sigma receptor function to PET scanning ligands, which have allowed visualization of sigma receptors in mammalian brain.